MS9117 | LSD1 PROTAC | Probechem Biochemicals

Chemical Structure : MS9117

MS9117 (MS-9117)

Catalog No.: PC-24632Not For Human Use, Lab Use Only.

MS9117 is a potent, selective CRBN-based LSD1 PROTAC degrader (DC50<40 nM in THP-1 cells), effectively degrades LSD1 in a concentration-, time-, and proteasome-dependent manner.

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Biological Activity

MS9117 is a potent, selective CRBN-based LSD1 PROTAC degrader (DC50<40 nM in THP-1 cells), effectively degrades LSD1 in a concentration-, time-, and proteasome-dependent manner.

MS9117 (40 nM) induced more than 50% degradation of LSD1, while 50 nM resulted in complete degradation in THP-1 cells.

LSD1 degradation induced by MS9117 is dependent on binding to LSD1 and the E3 ligase CRBN.

MS9117 shows cell growth inhibition effect on THP-1 cells with EC50 of 49 nM.

MS9117 selective degrades LSD1 with no effect on IKZF1 and GSPT1 levels.

MS9117 effectively inhibits proliferation and promotes differentiation of THP-1 leukemic cells, with greater potency than LSD1 enzymatic inhibitors, such as IMG-7289, CC-90011, and TAK-418.

Physicochemical Properties

M.Wt	938.95
Formula	C46H48F2N10O10
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-(2-(4-aminopiperidin-1-yl)-4-(4-cyano-3-fluorophenyl)-5-(3-fluoro-4-methoxyphenyl)-6-oxopyrimidin-1(6H)-yl)-N-(2-(2-(2-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)acetamido)ethoxy)ethoxy)ethyl)acetamide

References

1. Hosseini A, et al. Proc Natl Acad Sci U S A. 2025 May 20;122(20):e2425812122.

MS9117 (MS-9117)

Biological Activity

Physicochemical Properties

References

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